TWI615400B - ５'-經取代核苷化合物 - Google Patents

５'-經取代核苷化合物 Download PDF

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Publication number
TWI615400B
TWI615400B TW105112724A TW105112724A TWI615400B TW I615400 B TWI615400 B TW I615400B TW 105112724 A TW105112724 A TW 105112724A TW 105112724 A TW105112724 A TW 105112724A TW I615400 B TWI615400 B TW I615400B
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TW
Taiwan
Prior art keywords
mixture
mmol
pyrimidin
compound
cancer
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TW105112724A
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English (en)
Chinese (zh)
Other versions
TW201712022A (zh
Inventor
古勒莫Ｓ 蔻茲
卡洛 羅伯特 達恩奇
麥克 約翰 葛洛干
安東尼奧 洛德里古茲 賀古塔
詹姆士 安德魯 傑米森
布萊恩 摩根 華森
提摩西 安德魯 伍茲
沙海迪 奎永 邦戴
Original Assignee
美國禮來大藥廠
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Publication of TW201712022A publication Critical patent/TW201712022A/zh
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Publication of TWI615400B publication Critical patent/TWI615400B/zh

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/14—Pyrrolo-pyrimidine radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Saccharide Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
TW105112724A 2015-05-04 2016-04-22 ５'-經取代核苷化合物 TWI615400B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15382225 2015-05-04
??15382225.9 2015-05-04

Publications (2)

Publication Number Publication Date
TW201712022A TW201712022A (zh) 2017-04-01
TWI615400B true TWI615400B (zh) 2018-02-21

Family

ID=53177322

Family Applications (1)

Application Number Title Priority Date Filing Date
TW105112724A TWI615400B (zh) 2015-05-04 2016-04-22 ５'-經取代核苷化合物

Country Status (25)

Country Link
US (1) US9840532B2 (es)
EP (1) EP3292128A1 (es)
JP (2) JP6181889B1 (es)
KR (1) KR20170132871A (es)
CN (1) CN107580602A (es)
AR (1) AR104326A1 (es)
AU (1) AU2016258485A1 (es)
BR (1) BR112017020336A2 (es)
CA (1) CA2981097A1 (es)
CL (1) CL2017002637A1 (es)
CO (1) CO2017010727A2 (es)
CR (1) CR20170443A (es)
DO (1) DOP2017000255A (es)
EA (1) EA201792169A1 (es)
EC (1) ECSP17072987A (es)
HK (1) HK1244007A1 (es)
IL (1) IL254409A0 (es)
MA (1) MA42036A (es)
MX (1) MX2017014001A (es)
PE (1) PE20180231A1 (es)
PH (1) PH12017502002A1 (es)
SG (1) SG11201708345XA (es)
TN (1) TN2017000459A1 (es)
TW (1) TWI615400B (es)
WO (1) WO2016178870A1 (es)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20170119705A (ko) * 2015-02-24 2017-10-27 화이자 인코포레이티드 항암제로서 유용한 치환된 뉴클레오시드 유도체
WO2018139181A1 (ja) * 2017-01-27 2018-08-02 国立大学法人 宮崎大学 抗がん剤、抗がん剤のスクリーニング方法、がんに対する有効性判定キット及びがんに対する有効性判定方法
WO2018152548A1 (en) 2017-02-20 2018-08-23 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
WO2018152501A1 (en) 2017-02-20 2018-08-23 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
WO2018160855A1 (en) 2017-03-01 2018-09-07 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
EP3665179B1 (en) * 2017-08-09 2021-06-09 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
WO2019084470A1 (en) 2017-10-26 2019-05-02 Prelude Therapeutics, Incorporated SELECTIVE INHIBITORS OF THE PROTEIN ARGININE METHYLTRANSFERASE 5 (PRMT5)
IL274936B2 (en) 2017-12-13 2023-09-01 Lupin Ltd Transmuted heterocyclic bicyclic compounds as prmt5 inhibitors
KR20200132916A (ko) 2018-03-14 2020-11-25 프렐루드 테라퓨틱스, 인코포레이티드 단백질 아르기닌 메틸트랜스퍼라제 5(prmt5)의 선택적 억제제
US10711007B2 (en) 2018-03-14 2020-07-14 Prelude Therapeutics Incorporated Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)
JP7337539B2 (ja) * 2018-06-21 2023-09-04 メディヴィル・アクチエボラーグ 白血病療法のための塩基修飾シチジンヌクレオチド
WO2020033285A1 (en) * 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
MX2021009796A (es) * 2019-02-13 2021-09-08 Prelude Therapeutics Inc Inhibidores selectivos de la proteina arginina metiltransferasa 5 (prmt5).
RS64972B1 (sr) 2019-06-10 2024-01-31 Lupin Ltd Inhibitori prmt5
GEP20247638B (en) 2019-10-22 2024-07-10 Lupin Ltd Pharmaceutical combination of prmt5 inhibitors
EP4069698A1 (en) 2019-12-03 2022-10-12 Lupin Limited Substituted nucleoside analogs as prmt5 inhibitors
GB202117230D0 (en) 2021-11-29 2022-01-12 Argonaut Therapeutics Ltd Peptide vaccine
GB202203588D0 (en) 2022-03-15 2022-04-27 Argonaut Therapeutics Ltd Cancer diagnostic
CN116211869B (zh) * 2022-12-07 2023-08-01 浙江省肿瘤医院 含dna损伤修复抑制剂的药物混合物及混合方法、用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1384834A (zh) * 1999-08-27 2002-12-11 Icn药品公司 吡咯并[2,3－d]嘧啶核苷类似物
WO2007069923A1 (en) * 2005-12-15 2007-06-21 Industrial Research Limited Deazapurine analogs of 1'-aza-l-nucleosides

Family Cites Families (9)

* Cited by examiner, † Cited by third party
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US9044432B2 (en) 2009-12-22 2015-06-02 Ohio State Innovation Foundation Compositions and methods for cancer detection and treatment
US9416154B2 (en) * 2011-07-13 2016-08-16 Merck Sharp & Dohme Corp. 5′-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
WO2014100730A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
US20150344457A1 (en) 2012-12-21 2015-12-03 Epizyme, Inc. Methods of inhibiting prmt5
JP2016505597A (ja) 2012-12-21 2016-02-25 エピザイム，インコーポレイティド Ｐｒｍｔ５阻害剤およびその使用
US9365555B2 (en) * 2012-12-21 2016-06-14 Epizyme, Inc. PRMT5 inhibitors and uses thereof
US9908887B2 (en) 2012-12-21 2018-03-06 Epizyme, Inc. PRMT5 inhibitors and uses thereof
US8993555B2 (en) 2012-12-21 2015-03-31 Epizyme, Inc. PRMT5 inhibitors and uses thereof
KR20170119705A (ko) * 2015-02-24 2017-10-27 화이자 인코포레이티드 항암제로서 유용한 치환된 뉴클레오시드 유도체

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1384834A (zh) * 1999-08-27 2002-12-11 Icn药品公司 吡咯并[2,3－d]嘧啶核苷类似物
WO2007069923A1 (en) * 2005-12-15 2007-06-21 Industrial Research Limited Deazapurine analogs of 1'-aza-l-nucleosides

Also Published As

Publication number Publication date
CO2017010727A2 (es) 2018-01-31
JP2017525667A (ja) 2017-09-07
CL2017002637A1 (es) 2018-04-20
JP2017125029A (ja) 2017-07-20
CA2981097A1 (en) 2016-11-10
MA42036A (fr) 2018-03-14
TW201712022A (zh) 2017-04-01
PH12017502002A1 (en) 2018-03-26
MX2017014001A (es) 2018-03-16
EP3292128A1 (en) 2018-03-14
TN2017000459A1 (en) 2019-04-12
EA201792169A1 (ru) 2018-03-30
KR20170132871A (ko) 2017-12-04
HK1244007A1 (zh) 2018-07-27
PE20180231A1 (es) 2018-01-31
IL254409A0 (en) 2017-11-30
JP6181889B1 (ja) 2017-08-16
DOP2017000255A (es) 2018-01-15
CN107580602A (zh) 2018-01-12
AU2016258485A1 (en) 2017-10-12
CR20170443A (es) 2017-11-07
BR112017020336A2 (pt) 2019-05-14
ECSP17072987A (es) 2018-02-28
SG11201708345XA (en) 2017-11-29
WO2016178870A1 (en) 2016-11-10
AR104326A1 (es) 2017-07-12
US20160326208A1 (en) 2016-11-10
US9840532B2 (en) 2017-12-12

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